Title of article :
Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists
Author/Authors :
James E. Dowling، نويسنده , , Jeffrey T. Vessels، نويسنده , , Serajul Haque، نويسنده , , He Xi Chang، نويسنده , , Kurt van Vloten، نويسنده , , Gnanasambandam Kumaravel، نويسنده , , Thomas Engber، نويسنده , , Xiaowei Jin، نويسنده , , Deepali Phadke، نويسنده , , Joy Wang، نويسنده , , Eman Ayyub، نويسنده , , Russell C. Petter، نويسنده ,
Abstract :
Potent and selective antagonists of the adenosine A2A receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the preparation, by a novel route, of A2A receptor antagonists containing the [1,2,4]triazolo[1,5-a]pyrazine nucleus, which is isomeric with the [1,2,4]triazolo[1,5-c]pyrimidine core of a series of known A2A antagonists with in vivo activity in animal models of Parkinson’s disease.
